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5-羧酰胺色胺马来酸盐

5-羧酰胺色胺马来酸盐用途

5-Carboxamidotryptamine maleate (5-CT maleate) 是一种有效的 5-HT1A,5-HT1B,5-HT1D,5-HT5 和 5-HT7 受体激动剂。

5-羧酰胺色胺马来酸盐名称

[ CAS 号 ]:
74885-72-6

[ 中文名 ]:
5-羧酰胺色胺马来酸盐

[ 英文名 ]:
5-Carboxamidotryptamine maleate

[英文别名 ]:

MFCD00069224

5-羧酰胺色胺马来酸盐生物活性

[ 描述 ]:

5-Carboxamidotryptamine maleate (5-CT maleate) 是一种有效的 5-HT1A,5-HT1B,5-HT1D,5-HT5 和 5-HT7 受体激动剂。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT1A Receptor

5-HT1B Receptor

5-HT1D Receptor

5-HT5 Receptor

5-HT7 Receptor

[体外研究]

与牛黑质5-HT1D位点结合的[3H]-5-Carboxamidoryptamine(5-CT)具有快速、可逆和饱和的特点,表现出高亲和力(Kd=0.38nm)和低非特异性结合[2]。在牛黑质中,[3H]-5-甲酰胺三嗪(5-CT)标记的结合位点数量与[3H]-5-Carboxamidoryptamine(分别为403和362fmol/mg蛋白质)的结合位点,并且结合对鸟嘌呤核苷酸敏感[2]。

[体内研究]

暴露于硬脑膜的外用5-卡波胺(0.01-1000μM)可使麻醉Wistar大鼠的中脑膜动脉舒张压降低,脑膜血流量发生变化,传导率增加(即扩张)(5-羟色胺耗竭,用20 mg/kg皮质酮治疗)[1]。

[参考文献]

[1]. E Martínez-García, et al. 5-HT7 receptor-mediated meningeal dilatation induced by 5-carboxamidotryptamine in rats is not altered by 5-HT depletion and chronic corticosterone treatment. Proc West Pharmacol Soc. 2011;54:57-61.

[2]. H P Nowak, et al. [3H]-5-carboxamidotryptamine labels 5-HT1D binding sites in bovine substantia nigra. Br J Pharmacol. 1993 Aug;109(4):1206-11.

[3]. J Yamada, et al. Effects of the non-selective 5-HT receptor agonist, 5-carboxamidotryptamine, on plasma glucose levels in rats. Eur J Pharmacol. 1998 Oct 16;359(1):81-6.

5-羧酰胺色胺马来酸盐物理化学性质

[ 分子式 ]:
C₁₅H₁₇N₃O₅

[ 分子量 ]:
319.31

[ 外观性状 ]:
固体

[ 储存条件 ]:
-20°C

5-羧酰胺色胺马来酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

5-羧酰胺色胺马来酸盐文献

GR-127935-sensitive mechanism mediating hypotension in anesthetized rats: are 5-HT5B receptors involved?

J. Cardiovasc. Pharmacol. 65(4) , 335-41, (2015)

The 5-HT1B/1D receptor antagonist, GR-127935, inhibits hypotensive responses produced by the 5-HT1A, 5-HT1B/1D and 5-HT7 receptor agonist, and 5-HT5A/5B receptor ligand, 5-carboxamidotryptamine (5-CT)...

Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.

Bioorg. Med. Chem. 22(21) , 6026-38, (2014)

A series of 9-disubstituted N-(9H-fluorene-2-carbonyl)guanidine derivatives have been discovered as potent and orally active dual 5-HT(2B) and 5-HT(7) receptor antagonists. Upon screening several comp...

The serotonin receptor 5-HT₇R regulates the morphology and migratory properties of dendritic cells.

J. Cell Sci. 128 , 2866-80, (2015)

Dendritic cells are potent antigen-presenting cells endowed with the unique ability to initiate adaptive immune responses upon inflammation. Inflammatory processes are often associated with an increas...

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